Anti-tumor activity of N-thiolated beta-lactam antibiotics.

An ongoing strategy for cancer treatment is selective induction of apoptosis in cancer over normal cells. N-thiolated beta-lactams were found to induce DNA damage, growth arrest and apoptosis in cultured human cancer cells. However, whether these compounds have a similar effect in vivo has not been studied. We report here that treatment with the beta-lactam L-1 caused a significant inhibition of tumor growth in a breast cancer xenograft mouse model, associated with induction of DNA damage and apoptosis in vivo. These results suggest that the synthetic antibiotic N-thiolated beta-lactams hold great potential to be developed as novel anti-cancer drugs.